Synthesis and Biological Evaluation of 2-Substituted Quinoline 6-Carboxamides as Potential mGluR1 Antagonists for the Treatment of Neuropathic Pain

Title
Synthesis and Biological Evaluation of 2-Substituted Quinoline 6-Carboxamides as Potential mGluR1 Antagonists for the Treatment of Neuropathic Pain
Authors
김영희손지원김주현백두종이용섭임은정이재균배애님민선준조용서
Keywords
glutamate; metabotropic glutamate receptor (mGluR); quinoline; neuropathic pain; spinal nerve ligation (SNL) model
Issue Date
2014-06
Publisher
Chemical & pharmaceutical bulletin
Citation
VOL 62, NO 6, 508-518
Abstract
A series of 2-amino and 2-methoxy quinoline-6-carboxamide derivatives have been synthesized and their metabotropic glutamate receptor type 1 (mGluR1) antagonistic activities were evaluated in a functional cell-based assay. The compound 13c showed the highest potency with IC50 value of 2.16 μM against mGluR1. Finally, in vivo evaluation of 13c in the rat spinal nerve ligation (SNL) model exhibited weak analgesic effects with regard to both mechanical allodynia and cold allodynia.
URI
http://pubs.kist.re.kr/handle/201004/48258
ISSN
00092363
Appears in Collections:
KIST Publication > Article
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